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	靶向EGFR的新型喹啉类衍生物抗食管癌作用的特征; Antitumor effects of a novel chloroquinoline derivative as EGFR inhibitor on human esophageal carcinoma
	王雪玉 ; 邱飞 ; 唐明清 ; 吴振 ; 张勇 ; 王立强
	2014-06-05
关键词	4-取代-7氯喹啉衍生物 分子对接 表皮生长因子受体 食管癌 4-substituent-7-chloroquinoline derivative docking EGFR esophageal cancer
英文摘要	目的:评价Egfr抑制剂4-取代-7氯喹啉衍生物(TW9183)的体内外抗肿瘤生物活性。方法:采用分子对接技术探讨其与Egfr之间的相互作用模式,蛋白免疫印迹法评价在蛋白水平的直接作用,体外细胞生物学及体内裸鼠移植瘤模型探讨TW9183的活性。结果:Egfr受体的氨基酸残基MET769,PrO770,lyS721可与TW9183间形成氢键,蛋白印免疫迹法表明化合物抑制Egfr的磷酸化;体外细胞实验显示TW9183有明显抑制食管癌细胞增殖、周期阻滞于g2/M期及促进凋亡的效果;裸鼠食管癌移植瘤模型验证其在体内同样具有抑制肿瘤生长促进凋亡的作用。结论:TW9183在体内外实验中显示具有潜在的抗食管癌作用。; Objective: To explore the underlying mechanism of 4-substituent-7-chloroquinoline derivative(TW9183),which has a selective anti-tumor effect in vitro and in vivo.Methods: Docking simulation was performed to position compounds into the EGFR structure active site to determine a possible binding model.We also used Western blot assay to directly evaluate the interaction.Cell cultures and tumor xenografts were utilized to test the effect of TW9183.Results: TW9183 was nice bound to the EGFR with the amino hydrogens of MET769, PRO770 and LYS721,forming optimal H-bonds interaction.Western blot assay showed that the compound inhibited EGFR phosphorylation.TW9183 treatment increased typical apoptosis and the number of cells in the G2/ M phase in ECA-109 cells.In ECA-109 xenograft model in nude mice,TW9183 inhibited tumor growth and promoted apoptosis.Conclusion: TW9183 has potential antitumor activity in vitro and in vivo.; 泉州市科技计划重点项目(2013Z35)
语种	zh_CN
内容类型	期刊论文
源URL	[http://dspace.xmu.edu.cn/handle/2288/123457]
专题	药学院－已发表论文
推荐引用方式 GB/T 7714	王雪玉,邱飞,唐明清,等. 靶向EGFR的新型喹啉类衍生物抗食管癌作用的特征, Antitumor effects of a novel chloroquinoline derivative as EGFR inhibitor on human esophageal carcinoma[J],2014.
APA	王雪玉,邱飞,唐明清,吴振,张勇,&王立强.(2014).靶向EGFR的新型喹啉类衍生物抗食管癌作用的特征..
MLA	王雪玉,et al."靶向EGFR的新型喹啉类衍生物抗食管癌作用的特征".(2014).

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